HRP20201107T1 - Heteroaryl amides as inhibitors of protein aggregation - Google Patents

Heteroaryl amides as inhibitors of protein aggregation Download PDF

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HRP20201107T1
HRP20201107T1 HRP20201107TT HRP20201107T HRP20201107T1 HR P20201107 T1 HRP20201107 T1 HR P20201107T1 HR P20201107T T HRP20201107T T HR P20201107TT HR P20201107 T HRP20201107 T HR P20201107T HR P20201107 T1 HRP20201107 T1 HR P20201107T1
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pharmaceutically acceptable
acceptable salt
nitrogen
substituted
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HRP20201107TT
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Emily M. Stocking
Wolfgang Wrasidlo
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UCB Biopharma SRL
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Claims (17)

1. Spoj sa formulom (I): [image] gdje: R1 je H, halo, C1-4alkil, ili CF3; R2 je -CF3, ili C1-4alkil nesupstituiran ili supstituiran sa halo ili -CF3; A je 5-člani heteroaril prsten; Y je odsutno ili je C1-4alkilen; gdje Y je odsutno: R3 i R4 zajedno sa dušikom za koji su vezani formiraju monociklični heterocikloalkil prsten, nesupstituiran ili supstituiran sa C1-4alkilom; i gdje Y je C1-4alkilen: R3 i R4 zajedno sa dušikom za koji su vezani formiraju monociklični heterocikloalkil prsten, nesupstituiran ili supstituiran sa C1-4alkilom; ili R3 i Y zajedno sa dušikom za koji R3 je vezan formiraju monociklični heterocikloalkil prsten, i R4 je H ili C1-4alkil; ili farmaceutski prihvatljiva sol istog.1. Compound with formula (I): [image] where: R 1 is H, halo, C 1-4 alkyl, or CF 3 ; R 2 is -CF 3 , or C 1-4 alkyl unsubstituted or substituted with halo or -CF 3 ; A is a 5-membered heteroaryl ring; Y is absent or is C1-4 alkylene; where Y is absent: R3 and R4 together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl ring, unsubstituted or substituted with C1-4alkyl; and where Y is C1-4alkylene: R3 and R4 together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl ring, unsubstituted or substituted with C1-4alkyl; or R 3 and Y together with the nitrogen to which R 3 is attached form a monocyclic heterocycloalkyl ring, and R 4 is H or C 1-4 alkyl; or a pharmaceutically acceptable salt thereof. 2. Spoj u skladu sa patentnim zahtjevom 1, ili farmaceutski prihvatljiva sol istog, gdje: R1 je H, fluoro, kloro, bromo, metil, etil, propil, izopropil, butil, izobutil, sek-butil, ili terc-butil; ili R1 je H ili fluoro.2. A compound according to claim 1, or a pharmaceutically acceptable salt thereof, where: R 1 is H, fluoro, chloro, bromo, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, or tert-butyl; or R 1 is H or fluoro. 3. Spoj u skladu sa patentnim zahtjevom 1 ili 2, ili farmaceutski prihvatljiva sol istog, gdje: R2 je -CF3; ili R2 je metil, etil, propil, izopropil, butil, izobutil, sek-butil, ili terc-butil, svaki nesupstituiran ili supstituiran sa fluoro, kloro, bromo, ili -CF3; ili R2 je C1-4alkil po izboru supstituiran sa halo ili -CF3; ili R2 je C3-4alkil, nesupstituiran ili supstituiran sa fluoro ili -CF3; ili R2 je butil; ili R2 je propil supstituiran sa -CF3.3. A compound according to claim 1 or 2, or a pharmaceutically acceptable salt thereof, where: R 2 is -CF 3 ; or R 2 is methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, or tert-butyl, each unsubstituted or substituted with fluoro, chloro, bromo, or -CF 3 ; or R 2 is C 1-4 alkyl optionally substituted with halo or -CF 3 ; or R 2 is C 3-4 alkyl, unsubstituted or substituted with fluoro or -CF 3 ; or R 2 is butyl; or R 2 is propyl substituted with -CF 3 . 4. Spoj u skladu sa bilo kojim od patentnih zahtjeva 1 do 3, ili farmaceutski prihvatljiva sol istog, gdje: A je 5-člani heteroaril prsten sa dva ili tri atoma prstena koja su heteroatomi; ili A je 5- člani heteroaril prsten sa dva nesusjedna atoma prstena koja su heteroatomi; ili A je tiazol, tiadiazol, oksazol, imidazol, ili triazol; ili A je tiazol ili tiadiazol; ili A je tiazol.4. A compound according to any of claims 1 to 3, or a pharmaceutically acceptable salt thereof, where: A is a 5-membered heteroaryl ring with two or three ring atoms being heteroatoms; or A is a 5-membered heteroaryl ring with two nonadjacent ring atoms that are heteroatoms; or A is thiazole, thiadiazole, oxazole, imidazole, or triazole; or A is thiazole or thiadiazole; or A is thiazole. 5. Spoj u skladu sa bilo kojim od patentnog zahtjeva 1 do 4, ili farmaceutski prihvatljiva sol istog, gdje: Y je odsutno; ili Y je -CH2-, -CH2CH2-, -CH(CH3)-, -(CH2)3-, -C(CH3)2-, -(CH2)4-, -CH((CH2)2CH3)-, -CH(CH(CH3)2)-, -CH(CH2CH3)CH2-, -CH(CH3)CH(CH3)-, -CH(CH3)(CH2)2-, ili -CH2CH(CH3)CH2-; ili Y je -CH2-, -CH2CH2-, ili -CH(CH3)-; ili Y je -CH2CH2-.5. A compound according to any of claims 1 to 4, or a pharmaceutically acceptable salt thereof, where: Y is absent; or Y is -CH2-, -CH2CH2-, -CH(CH3)-, -(CH2)3-, -C(CH3)2-, -(CH2)4-, -CH((CH2)2CH3)-, - CH(CH(CH3)2)-, -CH(CH2CH3)CH2-, -CH(CH3)CH(CH3)-, -CH(CH3)(CH2)2-, or -CH2CH(CH3)CH2-; or Y is -CH2-, -CH2CH2-, or -CH(CH3)-; or Y is -CH2CH2-. 6. Spoj u skladu sa bilo kojim od patentnog zahtjeva 1 do 5, ili farmaceutski prihvatljiva sol istog, gdje: R3 i R4 su zajedno sa dušikom za koji su vezani formiraju monociklični heterocikloalkil prsten, nesupstituiran ili supstituiran sa C1-4alkilom; ili R3 i R4 zajedno sa dušikom za koji su vezani formiraju azetidin, pirolidin, piperidin, azepin, piperazin, morfolin, tiomorfolin, ili 1,1-diokso-tiomorfolin, svaki nesupstituiran ili supstituiran sa C1-4alkilom; ili R3 i R4 zajedno sa dušikom za koji su vezani formiraju piperazin, morfolin, ili pirolidin, svaki nesupstituiran ili supstituiran sa C1-4alkilom; ili R3 i R4 zajedno sa dušikom za koji su vezani formiraju piperazin ili morfolin, svaki nesupstituiran ili supstituiran sa C1-4alkilom; ili R3 i R4 zajedno sa dušikom za koji su vezani formiraju piperazin, nesupstituiran ili supstituiran sa C1-4alkilom; ili R3 i R4 zajedno sa dušikom za koji su vezani formiraju piperazin ili 4-metil-piperazin.6. A compound according to any of claims 1 to 5, or a pharmaceutically acceptable salt thereof, where: R3 and R4 together with the nitrogen to which they are attached form a monocyclic heterocycloalkyl ring, unsubstituted or substituted with C1-4alkyl; or R 3 and R 4 together with the nitrogen to which they are attached form azetidine, pyrrolidine, piperidine, azepine, piperazine, morpholine, thiomorpholine, or 1,1-dioxo-thiomorpholine, each unsubstituted or substituted with C 1-4 alkyl; or R 3 and R 4 together with the nitrogen to which they are attached form a piperazine, morpholine, or pyrrolidine, each unsubstituted or substituted with C 1-4 alkyl; or R 3 and R 4 together with the nitrogen to which they are attached form piperazine or morpholine, each unsubstituted or substituted with C 1-4 alkyl; or R3 and R4 together with the nitrogen to which they are attached form piperazine, unsubstituted or substituted with C1-4alkyl; or R3 and R4 together with the nitrogen to which they are attached form piperazine or 4-methyl-piperazine. 7. Spoj u skladu sa bilo kojim od patentnog zahtjeva 1 do 5, ili farmaceutski prihvatljiva sol istog, gdje: Y je C1-4alkilen, R3 i Y zajedno sa dušikom za koji R3 je vezan formiraju monociklični heterocikloalkil prsten, i R4 je H ili C1-4alkil; ili Y je C1-4alkilen, R3 i Y zajedno sa dušikom za koji R3 je vezan formiraju pirolidin ili piperidin.7. A compound according to any of claims 1 to 5, or a pharmaceutically acceptable salt thereof, where: Y is C1-4alkylene, R3 and Y together with the nitrogen to which R3 is attached form a monocyclic heterocycloalkyl ring, and R4 is H or C1-4alkyl; or Y is C1-4alkylene, R3 and Y together with the nitrogen to which R3 is attached form pyrrolidine or piperidine. 8. Spoj u skladu sa patentnim zahtjevom 7, ili farmaceutski prihvatljiva sol istog, gdje: R4 je H ili metil.8. A compound according to claim 7, or a pharmaceutically acceptable salt thereof, where: R4 is H or methyl. 9. Spoj u skladu sa patentnim zahtjevom 1, ili farmaceutski prihvatljiva sol istog, gdje: R1 je H, R2 je C1-4alkil, A je tiazol, Y je odsutno ili je etilen, i R3 i R4 zajedno sa dušikom za koji su vezani formiraju N-metilpiperazin.9. A compound according to claim 1, or a pharmaceutically acceptable salt thereof, where: R1 is H, R2 is C1-4alkyl, A is thiazole, Y is absent or is ethylene, i R3 and R4 together with the nitrogen to which they are attached form N-methylpiperazine. 10. Spoj u skladu sa bilo kojim od patentnog zahtjeva 1 do 9, ili farmaceutski prihvatljiva sol istog, gdje: R2 je u "R" stereokemijskoj konfiguraciji; ili R2 je u "S" stereokemijskoj konfiguraciji.10. A compound according to any of claims 1 to 9, or a pharmaceutically acceptable salt thereof, where: R 2 is in the "R" stereochemical configuration; or R 2 is in the "S" stereochemical configuration. 11. Spoj u skladu sa patentnim zahtjevom 1, odabran od spoja sa sljedećim formulama, ili farmaceutski prihvatljiva sol istog: [image] [image] [image] 11. A compound according to claim 1, selected from compounds with the following formulas, or a pharmaceutically acceptable salt thereof: [image] [image] [image] 12. Spoj u skladu sa patentnim zahtjevom 1, odabran od spoja sa sljedećim formulama, ili farmaceutski prihvatljiva sol istog: [image] 12. A compound according to claim 1, selected from compounds with the following formulas, or a pharmaceutically acceptable salt thereof: [image] 13. Farmaceutska kompozicija koja sadrži (a) najmanje jedan spoj ili farmaceutski prihvatljivu sol istog u skladu sa bilo kojim od patentnih zahtjeva 1 do 12, i (b) farmaceutski prihvatljiv ekscipijens.13. A pharmaceutical composition containing (a) at least one compound or a pharmaceutically acceptable salt thereof according to any one of claims 1 to 12, and (b) a pharmaceutically acceptable excipient. 14. Farmaceutska kompozicija koja sadrži (a) najmanje jedan spoj ili farmaceutski prihvatljivu sol istog u skladu sa bilo kojim od patentnih zahtjeva 1 do 12, i (b) farmaceutski prihvatljiv ekscipijens gdje R2 je u suštini u "R" ili u suštini u "S" stereokemijskoj konfiguraciji.14. A pharmaceutical composition containing (a) at least one compound or a pharmaceutically acceptable salt thereof according to any one of claims 1 to 12, and (b) a pharmaceutically acceptable excipient where R2 is essentially in "R" or essentially in " S" stereochemical configuration. 15. Spoj ili farmaceutski prihvatljiva sol u skladu sa bilo kojim od patentnih zahtjeva 1 do 12 ili farmaceutska kompozicija u skladu sa patentnim zahtjevom 13 ili 14 za primjenu u liječenju bolesti ili medicinskog stanja koje je u vezi sa proteinskom agregacijom.15. A compound or a pharmaceutically acceptable salt according to any one of claims 1 to 12 or a pharmaceutical composition according to claim 13 or 14 for use in the treatment of a disease or medical condition related to protein aggregation. 16. Spoj, farmaceutski prihvatljiva sol, ili farmaceutska kompozicija za primjenu u skladu sa patentnim zahtjevom 15, gdje je bolest ili medicinsko stanje Alzheimerova bolest, Parkinsonova bolest, fronto-temporalna demencija, demencija sa Lewyevim tijelima (bolest Lewyevih tijela), Parkinsonova bolest sa demencijom, multipla sistemska atrofija, amiotrofična lateralna skleroza, Huntingtonova bolest, rak, melanom, ili inflamatorna bolest.16. A compound, a pharmaceutically acceptable salt, or a pharmaceutical composition for use according to claim 15, wherein the disease or medical condition is Alzheimer's disease, Parkinson's disease, fronto-temporal dementia, dementia with Lewy bodies (Lewy body disease), Parkinson's disease with dementia, multiple system atrophy, amyotrophic lateral sclerosis, Huntington's disease, cancer, melanoma, or inflammatory disease. 17. Metoda interferencije sa akumulacijom proteinskih ili peptidnih agregata u stanici, ili sprečavanja, usporavanja, preusmjeravanja, ili inhibiranja proteinske ili peptidne agregacije u stanici, koja obuhvaća stupanje u kontakt stanice sa efikasnom količinom najmanje jednog spoja ili farmaceutski prihvatljive soli u skladu sa bilo kojim od patentnih zahtjeva 1 do 12 ili farmaceutske kompozicije u skladu sa patentnim zahtjevom 13 ili 14, gdje je stupanje u kontakt in vitro ili ex vivo.17. A method of interfering with the accumulation of protein or peptide aggregates in a cell, or of preventing, slowing down, redirecting, or inhibiting protein or peptide aggregation in a cell, which comprises contacting the cell with an effective amount of at least one compound or a pharmaceutically acceptable salt in accordance with any from claims 1 to 12 or a pharmaceutical composition according to claim 13 or 14, where the contacting is in vitro or ex vivo.
HRP20201107TT 2014-01-29 2020-07-14 Heteroaryl amides as inhibitors of protein aggregation HRP20201107T8 (en)

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